MEDICINAL CHEMISTRY APPLIED TO PROBLEMS PROMINENT IN SENESCENCE

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The work on ligands for receptors of catecholamines resulted in the preparation of compounds which selectively lesion either beta-adrenoceptors or alpha one-adrenoceptors. The lesion process in question leads to irreversible deactivation of receptors located on the cell surface through alkylation with a ligand; there is no cellular death or necrosis in the tissue. The potential of the approach was demonstrated by work on the peripheral nervous system (performed within the Section) and by work on the central nervous system (performed at The Johns Hopkins University). Lesions in the periphery of rats lasted for about a week and there was no crossover into the central nervous system. Lesions in beta-adrenoceptors in the brains of rats were long lasting (greater then 30 days) and by choice of conditions could be localized to the proximity of the injection site. The work on solubilizers resulted in the successful experimental therapy of hypervitaminosis A. Also, the first steps have been initiated by the licensing office of the Department of Commerce to bring the new pharmaceutical form of sex hormones, which is based on the solubilizers developed at NIA, into practical use.